2010
DOI: 10.1016/j.ijpharm.2010.03.059
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Solubility enhancement of hydrophobic compounds by cosolvents: Role of solute hydrophobicity on the solubilization effect

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Cited by 78 publications
(26 citation statements)
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“…A number of formulation approaches have been used to improve water solubility of hydrophobic drugs. These include cyclodextrin complexation, co-solvent systems, salt-forming techniques, prodrug formation, particle size reduction and self-microemulsifying drug delivery systems (SMEDDS) (Brewster and Loftsson, 2007;Fleisher et al, 1996;Hintzen et al, 2014;McConville and Friend, 2013;Millard et al, 2002;Miyako et al, 2010;Serajuddin, 2007).…”
Section: Introductionmentioning
confidence: 99%
“…A number of formulation approaches have been used to improve water solubility of hydrophobic drugs. These include cyclodextrin complexation, co-solvent systems, salt-forming techniques, prodrug formation, particle size reduction and self-microemulsifying drug delivery systems (SMEDDS) (Brewster and Loftsson, 2007;Fleisher et al, 1996;Hintzen et al, 2014;McConville and Friend, 2013;Millard et al, 2002;Miyako et al, 2010;Serajuddin, 2007).…”
Section: Introductionmentioning
confidence: 99%
“…According to the assumption that the effect of solute‐solvent interactions in the mixture as the (volume fraction) weighted average of the interactions in pure solvents, Yalkowsky and co‐workers introduced the L‐L model, which can be expressed in the form lnx3=x1lnX1+x2lnX2=lnX2+σx1, where x 1 and x 2 are the mole fractions of cosolvent and water in binary solvent mixtures and X 1 , X 2 , and x 3 refers to the mole fraction solubility of solute in pure cosolvent, water, and binary solvent mixtures, respectively. σ =ln( X 1 / X 2 ) is the solubilization power of the cosolvent . From the expression of Equation , it can be found a straight line for ln x 3 as a function of cosolvent fraction, corresponding to the monotonic increasing as the cosolvent fraction increased…”
Section: Introductionmentioning
confidence: 99%
“…There are several models, namely, the log‐linear (L‐L) model, the modified Wilson (MW) model, mixture response surface model, and the Williams–Amidon (WA) model, have been published in literatures to correlate the solubility of solute (s) in cosolvent + water mixtures. A deep reviewing of these models has been performed by Jouyban in “Handbook of Solubility of Pharmaceuticals.”…”
Section: Introductionmentioning
confidence: 99%
“…Various cosolvents used include different grades of polyethylene glycols like PEG 100, PEG 200, PEG 300, PEG 400, and PEG 600; propylene glycols; glycerol; diethylene glycol monoethyl ether; pyrrolidones; glycofurol; alcohol; Soluphor P; Pharmasolve; etc. (27)(28)(29). The primary concern of a cosolventbased approach is the precipitation of solubilized drug upon dilution with aqueous fluids.…”
Section: Conventional Approachesmentioning
confidence: 99%